Patents Assigned to ArQule, Inc.
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Patent number: 9422283Abstract: The present application relates to salts of Compound A, 3-(3-(4-(1-aminocyclobutyl) phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine, solid state forms of Compound A free base or of salts of Compound A, amorphous forms of Compound A free base or of salts of Compound A, crystalline forms of Compound A free base or of salts of Compound A, polymorphs of Compound A free base or of salts of Compound A, and mesomorphs of Compound A free base or of salts of Compound A. The present application also relates to pharmaceutical compositions comprising these salts, solid state forms, amorphous forms, crystalline forms, polymorphs, or mesomorphs of Compound A free base or of salts of Compound A. The present application provides methods for preparing these salts, solid state forms, amorphous forms, crystalline forms, polymorphs, or mesomorphs of Compound A free base or of salts of Compound A.Type: GrantFiled: April 22, 2015Date of Patent: August 23, 2016Assignee: ArQule, Inc.Inventors: Craig Bates, Jianmin Mao, David Reed
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Patent number: 9180099Abstract: The present invention provides pyrroloquinolinyl-pyrrole-2,5-dione formulations and methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of the formulations containing pyrroloquinolinyl-pyrrole-2,5-dione compounds.Type: GrantFiled: July 6, 2012Date of Patent: November 10, 2015Assignee: ArQule Inc.Inventors: Hiroshi Yamakose, Takafumi Kato
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Patent number: 9012466Abstract: The present invention relates to substituted tricyclic pyrazolo-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted tricyclic pyrazolo-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: March 11, 2014Date of Patent: April 21, 2015Assignee: ArQule Inc.Inventors: Nivedita Namdev, Jianqiang Wang, Mark Ashwell, Audra Dalton, Jason Hill, Eugene Kelleher, Jeffrey Link, Rocio Palma, Sudharshan Eathiraj, Neil Westlund, Hui Wu, Rui-Yang Yang
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Patent number: 9000005Abstract: The present invention relates to highly-pure pyrroloquinolinyl-pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione, for example, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione, and pharmaceutically acceptable salts, solvates, and diastereomers thereof. The present invention also relates to methods for preparing highly-pure pyrroloquinolinyl-pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione, for example, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione, and pharmaceutically acceptable salts, solvates, and diastereomers thereof.Type: GrantFiled: March 7, 2013Date of Patent: April 7, 2015Assignee: ArQule, Inc.Inventors: Yoshitaka Nakamura, Jo Ooyama
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Patent number: 8962619Abstract: The present invention relates to substituted imidazopyridinyl-aminopyridine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl-aminopyridine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: November 8, 2013Date of Patent: February 24, 2015Assignee: ArQule, Inc.Inventors: Mark A. Ashwell, Chris Brassard, Anton Filikov, Jason Hill, Steffi Koerner, Jean-Marc Lapierre, Yanbin Liu, Nivedita Namdev, Robert Nicewonger, Rocio Palma, Manish Tandon, David Vensel, Akihisa Matsuda, Shin Iimura, Kenichi Yoshida, Takanori Yamazaki, Takahiro Kitamura, Takeshi Isoyama
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Patent number: 8906928Abstract: The present invention relates to substituted pyrazolo-pyrrolo-pyridine-dione compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted pyrazolo-pyrrolo-pyridine-dione compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: March 31, 2010Date of Patent: December 9, 2014Assignee: ArQule, Inc.Inventors: Jason Hill, Manish Tandon, Nivedita Namdev, Rocio Palma, Neil Westlund, Anton Filikov
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Patent number: 8871933Abstract: The present invention relates to a form 1 and form 2 polymorph of (?)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione. The present invention also relates to (?)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione compounds having a chiral purity greater than 99%, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising these (?)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione compounds.Type: GrantFiled: September 25, 2013Date of Patent: October 28, 2014Assignee: ArQule, Inc.Inventors: David P. Reed, Neil R. Barnes, John C. Kane, Christopher A. Lee, Jian-Xie Chen, Martin P. Redmon
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Patent number: 8815854Abstract: The present invention relates to substituted imidazopyridinyl compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: June 21, 2012Date of Patent: August 26, 2014Assignee: ArQule, Inc.Inventors: Mark A. Ashwell, Chris Brassard, Anton Filikov, Jason Hill, Steffi Koerner, Jean-Marc Lapierre, Yanbin Liu, Nivedita Namdev, Robert Nicewonger, Rocio Palma, Manish Tandon, David Vensel, Akihisa Matsuda, Shin Iimura, Yuko Yamamoto, Takeshi Isoyama
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Patent number: 8754078Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent.Type: GrantFiled: February 7, 2013Date of Patent: June 17, 2014Assignee: ArQule, Inc.Inventors: Chiang J. Li, Mark A. Ashwell, Jason Hill, Magdi M. Moussa, Neru Munshi
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Publication number: 20140031551Abstract: The present invention relates to a form 1 and form 2 polymorph of (?)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione. The present invention also relates to (?)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione compounds having a chiral purity greater than 99%, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising these (?)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione compounds.Type: ApplicationFiled: September 25, 2013Publication date: January 30, 2014Applicant: ArQule, Inc.Inventors: David P. Reed, Neil R. Barnes, John C. Kane, Christopher A. Lee, Jian-Xie Chen, Martin P. Redmon
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Patent number: 8614228Abstract: The present invention relates to quinone prodrug compositions and therapeutic methods using such prodrug compositions. Preferably, the quinone compounds of the invention are napthoquinone compounds such as ?-lapachone or ?-lapachone analogs. The quinone prodrug compositions of the invention exhibit improved solubility, stability, bioavailability, and pharmacokinetic properties, as well as improved plasma half-life in vivo.Type: GrantFiled: August 11, 2005Date of Patent: December 24, 2013Assignee: ArQule, Inc.Inventors: Mark A. Ashwell, Manish Tandon, Jean-Marc Lapierre, Yanbin Liu
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Patent number: 8609688Abstract: The present invention relates to substituted imidazopyridinyl-aminopyridine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl-aminopyridine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: June 21, 2012Date of Patent: December 17, 2013Assignee: ArQule, Inc.Inventors: Mark A. Ashwell, Chris Brassard, Anton Filikov, Jason Hill, Steffi Koerner, Jean-Marc Lapierre, Yanbin Liu, Nivedita Namdev, Robert Nicewonger, Rocio Palma, Manish Tandon, David Vensel, Akihisa Matsuda, Shin Iimura, Kenichi Yoshida, Takanori Yamazaki, Takahiro Kitamura, Takeshi Isoyama
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Patent number: 8580764Abstract: The present invention provides methods of treating a cell proliferative disorder, such as lung cancer and breast cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or a pyrroloquinolinyl-pyrrolidine-2,5-dione compound, such as (?)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione, in combination with a therapeutically effective amount of a second anti-proliferative agent, such as gemcitabine.Type: GrantFiled: July 1, 2011Date of Patent: November 12, 2013Assignee: ArQule, Inc.Inventors: Giovanni Abbadessa, Dennis S. France, Chang-Rung Chen, Thomas C. K. Chan
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Patent number: 8580803Abstract: The present invention relates to substituted pyrrolo-aminopyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted pyrrolo-aminopyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: December 29, 2010Date of Patent: November 12, 2013Assignee: ArQule, Inc.Inventors: Yanbin Liu, Nivedita Namdev, Rocio Palma, Manish Tandon, Jianqiang Wang, Hui Wu
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Patent number: 8575191Abstract: The present invention provides methods of treating non-small cell lung cancer by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound in combination with a therapeutically effective amount of an epidermal growth factor tyrosine kinase inhibitor.Type: GrantFiled: August 31, 2011Date of Patent: November 5, 2013Assignee: ArQule, Inc.Inventors: Yinpu Chen, Edward G. Garmey, Brian Schwartz
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Patent number: 8569331Abstract: The present invention relates to substituted benzo[f]imidazo[1,2-d]pyrido[2,3-b][1,4]diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzo[f]imidazo[1,2-d]pyrido[2,3-b][1,4]diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: November 1, 2011Date of Patent: October 29, 2013Assignee: ArQule, Inc.Inventors: Mark A. Ashwell, Sudharshan Eathiraj, Anton Filikov, Steffi Koerner, Jean-Marc Lapierre, Yanbin Liu, Rocio Palma, David Vensel, Shin Iimura, Akiko Shiina, Kenichi Yoshida, Takanori Yamazaki, Akihisa Matsuda
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Publication number: 20130281699Abstract: The present invention relates to highly-pure pyrroloquinolinyl-pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione, for example, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione, and pharmaceutically acceptable salts, solvates, and diastereomers thereof. The present invention also relates to methods for preparing highly-pure pyrroloquinolinyl-pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione, for example, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione, and pharmaceutically acceptable salts, solvates, and diastereomers thereof.Type: ApplicationFiled: March 7, 2013Publication date: October 24, 2013Applicant: ARQULE, INC.Inventors: Yoshitaka Nakamura, Jo Ooyama
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Patent number: 8563567Abstract: The present invention relates to substituted heterocyclic compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted heterocyclic compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: December 29, 2010Date of Patent: October 22, 2013Assignee: ArQule, Inc.Inventors: Syed M. Ali, Mark A. Ashwell, Yanbin Liu, Magdi Moussa, Jianqiang Wang, Hui Wu
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Patent number: 8552192Abstract: The present invention relates to a form 1 and form 2 polymorph of (?)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione. The present invention also relates to (?)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl) pyrrolidine-2,5-dione compounds having a chiral purity greater than 99%, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising these (?)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione compounds.Type: GrantFiled: December 22, 2010Date of Patent: October 8, 2013Assignee: ArQule, Inc.Inventors: David P. Reed, Neil R. Barnes, John C. Kane, Christopher A. Lee, Jian-Xie Chen, Martin P. Redmon
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Patent number: 8541407Abstract: The present invention relates to substituted benzo-pyrido-triazolo-diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzo-pyrido-triazolo-diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: March 31, 2011Date of Patent: September 24, 2013Assignee: ArQule, Inc.Inventors: Syed M. Ali, Mark A. Ashwell, Eugene Kelleher, Steffi Koerner, Jean-Marc Lapierre, Jeffrey S. Link, Yanbin Liu, Magdi Moussa, Rocio Palma, Manish Tandon, David Vensel, Neil Westlund, Hui Wu, Rui-Yang Yang